Compounds which can block the response to chemical...

Organic compounds -- part of the class 532-570 series – Organic compounds – Amino nitrogen containing

Reexamination Certificate

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Details

C562S444000, C562S445000, C562S448000, C514S563000, C514S616000

Reexamination Certificate

active

10515459

ABSTRACT:
The invention relates to compounds having formula (I), which can block the response to chemical substances or thermal stimuli or mediators of inflammation of nociceptors, a production method thereof and compositions containing same. According to the invention, Ar is a phenyl group substituted with one or more halogen groups; R1is amino, hydroxyl or thiol, all of which may or may not be substituted with formula (II) or with aliphatic or cyclic groups; R2is H or an alkyl, aryl, aralkyl or acyl group or formula (III); R3is H or formula (IV); R4and R6are H or an aliphatic or cyclic group; R5is H or formula (V); R7is H or an aliphatic or cyclic group; Z is amino, hydroxyl or thiol, all of which may or may not be substituted with aliphatic or cyclic groups; W is a linkage or formula (VI); X is a linkage or formula (VII); Y is amino which may or may not be substituted with formula (VIII) or an alkyl, aryl, aralkyl or acyl group; m, q and s can vary between 1 and 9 and n and p can vary between 1 and 10

REFERENCES:
patent: WO 02/30956 (2002-04-01), None
Carolina Garcia-Martinez, et al. “Attenuation of thermal nociception and hyperalgesia by VR1 blockers”PNAS, vol. 99, No. 4, Feb. 19, 2002, pp. 2374-2379.
Jacqueline A. Gibbons, et al. “Pharmacologic Characterization of CHIR 2279, an N-Substituted Glycine Peptoid wtih High-Affinity Binding for α1-Adrenoceptors”,Journal of Pharmacology and Experimental Therapeutics, vol. 277, No. 2, 1996, pp. 885-899.
John A. W. Kruijtzer, et al. “Solid-Phase Syntheses of Peptoids using Fmoc-Protected N-Substituted Glycines: The Syntheses of (Retro) Peptoids of Leu-Enkephalin and Substance P”Chem. Eur. J. 1998, No. 8, pp. 1570-1580.
Humet, M., et al., “A Positional Scanning Combinatorial Library of Peptoids As a Source of Biological Active Molecules: Identification of Antimicrobials”,J. Comb. Chem., 5:597-605 (2003).

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